The origins of inhalation therapy can be traced back to the early civilizations but this route of administration was relatively uncommon until recently. Direct delivery of drugs to the lung by inhalation for the treatment of respiratory disease grew rapidly in the second half of the 20th century as a result of the availability of effective asthma drugs in convenient, portable delivery systems. In the search for non-invasive delivery of biologics, it was discovered that the large highly absorptive surface area of the lung could be used for systemic delivery of proteins such as insulin. New delivery systems with efficiency and reproducibility to match the high cost and therapeutic constraints of biologics are currently in late stage clinical trials. Even small molecular weight drugs previously administered by injection are tested via the inhalation route either to provide non-invasively rapid onset of action, or to improve the therapeutic ratio for drugs acting in the lung. Gene therapy of pulmonary disease is still in its infancy but could provide valuable solutions to currently unmet medical needs. The beginning of the new millennium is therefore likely to witness development of many valuable therapeutic products delivered by inhalation.